Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/08/03 07:42:57」(JST)

wiki en

Pirenzepine (Gastrozepin), an M1 selective antagonist, is used in the treatment of peptic ulcers, as it reduces gastric acid secretion and reduces muscle spasm. It is in a class of drugs known as muscarinic receptor antagonists - acetylcholine being the neurotransmitter of the parasympathetic nervous system which initiates the rest-and-digest state (as opposed to fight-or-flight), resulting in an increase in gastric motility and digestion; whereas pirenzepine would inhibit these actions and cause decreased gastric motility leading to delayed gastric emptying and constipation.^[1] It has no effects on the brain and spinal cord as it cannot diffuse through the blood–brain barrier.

Pirenzepine has been investigated for use in myopia control.^[2]^[3]

It promotes the homodimerization or oligomerisation of M1 receptors.^[4]

References

^ Stolerman, Ian P. (2 August 2010). Encyclopedia of Psychopharmacology. Springer. p. 811. ISBN 978-3-540-68698-9. Retrieved 26 June 2013.
^ Czepita D (2005). "Fundamentals of modern treatment of myopia". Ann Acad Med Stetin. 51 (2): 5–9. PMID 16519089.
^ Walline JJ, Lindsley K, Vedula SS, Cotter SA, Mutti DO, Twelker JD (2011). "Interventions to slow progression of myopia in children". Cochrane Database Syst Rev (12): CD004916. doi:10.1002/14651858.CD004916.pub3. PMC 4270373. PMID 22161388.
^ Pediani JD, Ward RJ, Godin AG, Marsango S, Milligan G (2016): "Dynamic Regulation of Quaternary Organization of the M1 Muscarinic Receptor by Subtype-Selective Antagonist Drugs." J Biol Chem. PMID 27080256

This drug article relating to the gastrointestinal system is a stub. You can help Wikipedia by expanding it.

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. 小児における屈折異常 refractive errors in children

English Journal

Contribution of M and M muscarinic receptor subtypes to convulsions in fasted mice treated with scopolamine and given food.

Saygı Bacanak M, Aydın B, Cabadak H, Nurten A, Gören MZ, Enginar N.
Behavioural brain research. 2019 May;364()423-430.
Treatment of fasted mice and rats with the nonselective muscarinic antagonist, scopolamine or atropine, causes convulsions after food intake. This study evaluated the effect of fasting on the expression of M and M muscarinic receptors in the brain regions, the relationship between receptor expressio
PMID 29158113

Augmentation of Endogenous Acetylcholine Uptake and Cholinergic Facilitation of Hippocampal Long-Term Potentiation by Acetylcholinesterase Inhibition.

Masuoka T, Uwada J, Kudo M, Yoshiki H, Yamashita Y, Taniguchi T, Nishio M, Ishibashi T, Muramatsu I.
Neuroscience. 2019 Apr;404()39-47.
Hippocampal cholinergic activity enhances long-term potentiation (LTP) of synaptic transmission in intrahippocampal circuits and regulates cognitive function. We recently demonstrated intracellular distribution of functional M1-muscarinic acetylcholine receptors (mAChRs) and neuronal uptake of acety
PMID 30708046

Effects of time-of-day on inhibition of lens-induced myopia by quinpirole, pirenzepine and atropine in chicks.

Nickla DL, Jordan K, Yang J, Singh P.
Experimental eye research. 2019 Apr;181()5-14.
Injections of the D2 dopamine receptor agonist quinpirole or the acetylcholine muscarinic receptor antagonists pirenzepine and atropine prevent the development of negative-lens-induced myopia in chicks by inhibiting ocular growth. Because ocular growth is diurnally rhythmic, we hypothesized that the
PMID 30629959

Japanese Journal

モルヒネ誘発悪心・嘔吐,便秘に対するムスカリンM₁受容体拮抗薬の有用性

日本緩和医療薬学雑誌 8(2), 31-37, 2015-06
NAID 40020519297

Pharmacology : Vasomotor Effects of Acetylcholine, Bradykinin, Noradrenaline, 5-Hydroxytryptamine, Histamine and Angiotensin Ⅱ on the Mouse Basilar Artery

Journal of Veterinary Medical Science 76(10), 1339-1345, 2014
NAID 130004432214

Intracellular calcium level is an important factor influencing ion channel modulations by PLC-coupled metabotropic receptors in hippocampal neurons

Brain Research 1512, 9-21, 2013
NAID 120005302294

Related Pictures

Pirenzepine : Therapeutic uses, Dosage & Side Effects - DoctorAlerts Interventie mogelijkheden voor myopie ontwikkeling - ppt download Pirenzepine, [N-Methyl-3H]-, 1mCi (37MBq) | PerkinElmer Pirenzepine dihydrochloride ≥98% (TLC), powder | Sigma-Aldrich 21.drugs used in peptic ulcer Pirenzepine Hydrochloride tab 25mg : 100's｜Family Pharmacy Global Atropine substitutes

★リンクテーブル★

リンク元	「ムスカリン受容体拮抗薬」「ピレンゼピン」
拡張検索	「pirenzepine hydrochloride hydrate」「pirenzepine hydrochloride」

「ムスカリン受容体拮抗薬」

Pirenzepine
Systematic (IUPAC) name
	11-[(4-methylpiperazin-1-yl)acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one
Clinical data
AHFS/Drugs.com	Monograph
Identifiers
CAS Number	28797-61-7
ATC code	A02BX03 (WHO)
PubChem	CID 4848
IUPHAR/BPS	328
DrugBank	DB00670
ChemSpider	4682
UNII	3G0285N20N
KEGG	D08389
ChEBI	CHEBI:8247
ChEMBL	CHEMBL9967
Chemical data
Formula	C19H21N5O2
Molar mass	351.403 g/mol
	SMILES O=C3c1ccccc1N(C(=O)CN2CCN(C)CC2)c4ncccc4N3 ;
	InChI InChI=1S/C19H21N5O2/c1-22-9-11-23(12-10-22)13-17(25)24-16-7-3-2-5-14(16)19(26)21-15-6-4-8-20-18(15)24/h2-8H,9-13H2,1H3,(H,21,26) ; Key:RMHMFHUVIITRHF-UHFFFAOYSA-N ;
(verify)

　　[★]

英: muscarinic receptor antagonist
同: ムスカリン受容体遮断薬、抗ムスカリン様作用薬、antimuscarinic drug
関: ムスカリン受容体、アセチルコリン受容体

ベラドンナアルカロイド

気道閉塞性障害

イプラトロピウム ipratropium

散瞳薬

鎮痙薬

臭化ブチルスコポラミン scopolamine butylbromide

製品名：ブスコパン Buscopan

チキジウム tiquizium

抗潰瘍薬

パーキンソン病治療薬

「ピレンゼピン」

　　[★]

英: pirenzepine
化: 塩酸ピレンゼピン pirenzepine hydrochloride
商: ガストシオン、ガストロゼピン、ガタンプル、カロデリン、ストマゼピン、ピレンゼール、ピロデイン、ピン、ランクリック
関: ムスカリン性受容体、テレンゼピン; 消化性潰瘍用剤

抗潰瘍薬
三環系の化学構造

→　血液脳関門を通過しないので、中枢作用がない

特徴

消化管、尿路に対する作用が無く、散瞳、視力障害、循環器に対する作用もない (SPC.162)

M₁受容体特異的に作用する

薬理作用

胃粘膜壁細胞のムスカリン受容体に選択的に作用し胃酸分泌を抑制
迷走神経の胃酸分泌機能を特異的に抑制

「pirenzepine hydrochloride hydrate」

　　[★]

塩酸ピレンゼピン水和物

関: pirenzepine、pirenzepine hydrochloride

「pirenzepine hydrochloride」

　　[★]

塩酸ピレンゼピン

関: pirenzepine、pirenzepine hydrochloride hydrate

[Stolerman2010-1] Stolerman, Ian P. (2 August 2010). Encyclopedia of Psychopharmacology. Springer. p. 811. ISBN 978-3-540-68698-9. Retrieved 26 June 2013.

[2] Czepita D (2005). "Fundamentals of modern treatment of myopia". Ann Acad Med Stetin. 51 (2): 5–9. PMID 16519089.

[3] Walline JJ, Lindsley K, Vedula SS, Cotter SA, Mutti DO, Twelker JD (2011). "Interventions to slow progression of myopia in children". Cochrane Database Syst Rev (12): CD004916. doi:10.1002/14651858.CD004916.pub3. PMC 4270373. PMID 22161388.

[4] Pediani JD, Ward RJ, Godin AG, Marsango S, Milligan G (2016): "Dynamic Regulation of Quaternary Organization of the M1 Muscarinic Receptor by Subtype-Selective Antagonist Drugs." J Biol Chem. PMID 27080256

v t e Drugs for peptic ulcer and GERD/GORD (A02B)

H₂ antagonists ("-tidine")	Cimetidine Famotidine Lafutidine Lavoltidine (loxtidine) Niperotidine Nizatidine Ranitidine Roxatidine

Prostaglandins (E)/analogues ("-prost-")	Misoprostol Enprostil

Proton-pump inhibitors ("-prazole")	Dexlansoprazole Esomeprazole Ilaprazole Lansoprazole Omeprazole Pantoprazole Picoprazole Rabeprazole Tenatoprazole Timoprazole

Potassium-competitive acid blockers ("-prazan")	Linaprazan Revaprazan Soraprazan Vonoprazan

Others	Aceglutamide aluminum Acetoxolone Alginic acid Arbaclofen placarbil Carbenoxolone Cetraxate Gefarnate Lesogaberan Pirenzepine Proglumide Rebamipide Sucralfate Sulglicotide Telenzepine Teprenone Troxipide Zinc L-carnosine Zolimidine

Combinations	Bismuth subcitrate/metronidazole/tetracycline

See also: Helicobacter pylori* eradication protocols*

v t e Piperazines

Simple piperazines (no additional rings)	1-Cyclohexylpiperazine Aminoethylpiperazine Diethylcarbamazine HEPPS Midafotel Piperazine PIPES

Phenylpiperazines	Acaprazine Antrafenine Aripiprazole Batoprazine Bifeprunox BRL-15,572 Ciprofloxacin CSP-2503 Dapiprazole DCPP DMPP Diphenylpiperazine Dropropizine EGIS-12,233 Elopiprazole Eltoprazine Enpiprazole Ensaculin Etoperidone Flesinoxan Flibanserin Fluprazine Itraconazole Ketoconazole Levodropropizine Lorpiprazole mCPP Mefway MeOPP Mepiprazole Naftopidil Naluzotan Naphthylpiperazine Nefazodone Niaprazine Oxypertine Pardoprunox pCPP pFPP Posaconazole S-14,506 S-14,671 S-15,535 SB-258,585 SB-271,046 SB-357,134 SB-399,885 Sonepiprazole TFMPP Tolpiprazole Trazodone Urapidil Vesnarinone Vilazodone Vortioxetine WAY-100,135 WAY-100,635

Benzylpiperazines	2C-B-BZP Befuraline Bifeprunox Buclizine BZP Chlorbenzoxamine DBZP Fipexide Imatinib MBZP MDBZP Meclozine Methoxypiperamide Piberaline Piribedil Sunifiram Trimetazidine Vesnarinone

Diphenylalkylpiperazines (benzhydrylalkylpiperazines)	Almitrine Amperozide BRL-15,572 Buclizine BW373U86 Cetirizine Chlorbenzoxamine Chlorcyclizine Cinnarizine Clocinizine Cyclizine DBL-583 Diphenylmethylpiperazine Dotarizine DPI-221 DPI-287 DPI-3290 GBR-12,783 GBR-12,935 GBR-13,069 GBR-13,098 GBR-13,119 Hydroxyzine Lidoflazine Manidipine Meclozine Oxatomide SNC-80 Vanoxerine

Pyrimidinylpiperazines	Buspirone Dasatinib Eptapirone Gepirone Ipsapirone Piribedil Prazitone Pyrimidinylpiperazine Revospirone Tandospirone Tirilazad Trimazosin Umespirone Zalospirone

Pyridinylpiperazines	Atevirdine Azaperone Delavirdine Mirtazapine Pyridinylpiperazine

Benzo(iso)thiazolylpiperazines	Lurasidone Perospirone Revospirone Tiospirone Ziprasidone

Tricyclics (piperazine attached via side chain)	Amoxapine Clopenthixol Clorotepine Clozapine Cyanothepin Doclothepin Docloxythepin Flupentixol Fluphenazine Isofloxythepin Loxapine Meperathiepin Metitepine Octomethothepin Olanzapine Opipramol Oxyclothepin Oxyprothepin Peradithiepin Perathiepin Perazine Perphenazine Pirenzepine Prochlorperazine Thiethylperazine Thiothixene Trifluoperazine Trifluthepin Zuclopenthixol

Others/Uncategorized	6-Nitroquipazine Azimilide Cinepazet Cinepazic acid Cinepazide Cyclohexylpiperazine Hexocyclium Indinavir JNJ-7777120 Lodenafil Mirodenafil PB-28 Quipazine Ranolazine SA-4503 Sildenafil Tadalafil Vardenafil VUF-6002 Zipeprol

v t e Tricyclics

Classes	Acridine Anthracene Dibenzazepine Dibenzocycloheptene Dibenzodiazepine Dibenzothiazepine Dibenzothiepin Dibenzoxazepine Dibenzoxepin Phenothiazine Pyridazinobenzoxazine Pyridinobenzodiazepine Thioxanthene

Antidepressants (TCAs and TeCAs)	7-OH-Amoxapine Amezepine Amineptine Amitriptyline Amitriptylinoxide Amoxapine Aptazapine Azepindole Azipramine Batelapine Butriptyline Cianopramine Ciclazindol Ciclopramine Cidoxepin Clomipramine Cotriptyline Cyanodothiepin Demexiptiline Depramine/Balipramine Desipramine Dibenzepin Dimetacrine Dosulepin/Dothiepin Doxepin Enprazepine Esmirtazapine Fantridone Fluotracen Hepzidine Homopipramol Imipramine Imipraminoxide Intriptyline Iprindole Ketipramine Litracen Lofepramine Losindole Loxapine Maprotiline Mariptiline Mazindol Melitracen Metapramine Mezepine Mianserin Mirtazapine Monometacrine Naranol Nitroxazepine Nortriptyline Noxiptiline Octriptyline Opipramol Oxaprotiline Pipofezine Pirandamine Propizepine Protriptyline Quinupramine Setiptiline/Teciptiline Spiroxepin Tandamine Tampramine Tianeptine Tienopramine Trimipramine

Antihistamines	Azatadine Clobenzepam Cyproheptadine Dacemazine Deptropine Desloratadine Epinastine Etymemazine Fenethazine Hydroxyethylpromethazine Isopromethazine Isothipendyl Ketotifen Latrepirdine Loratadine Mebhydrolin Mequitazine Methdilazine Olopatadine Oxomemazine Phenindamine Pimethixene Promethazine Propiomazine Rupatadine Thiazinamium

Antipsychotics	Acetophenazine Alimemazine Amoxapine Asenapine Butaclamol Butaperazine Carfenazine (carphenazine) Carpipramine Chlorpromazine Chlorprothixene Ciclindole Citatepine Clocapramine Clomacran Clorotepine Clotiapine Clozapine Cyanothepin Doclothepin Docloxythepin Erizepine Flucindole Flumezapine Fluotracen Flupentixol Fluphenazine Gevotroline Homopipramol Isofloxythepin Levomepromazine/Methotrimeprazine Loxapine Maroxepin Meperathiepin Mesoridazine Metiapine Metitepine Metoxepin Mosapramine Naranol Octomethothepin Olanzapine Oxyclothepin Oxyprothepin Pentiapine Peradithiepin Perathiepin Perazine Perphenazine Periciazine Pinoxepin Piperacetazine Pipotiazine Piquindone Prochlorperazine Promazine Prothipendyl Quetiapine Savoxepin/Cipazoxapine Sulforidazine Tenilapine Thiethylperazine Thiopropazate Thioridazine Thiothixene Tilozepine Traboxopine Trifluoperazine Triflupromazine Trifluthepin Zotepine Zuclopenthixol

Anticonvulsants	Carbamazepine Dizocilpine Eslicarbazepine Eslicarbazepine acetate Etazepine Licarbazepine Oxcarbazepine Oxitriptyline Rispenzepine

Others	Adosopine Aminopromazine Atiprosin Beloxepin Carvedilol Cidoxepin Cyclobenzaprine Damotepine Darenzepine Elanzepine Methylene blue Monatepil Nuvenzepine Oxetorone Perlapine P7C3 Pinadoline Pirenzepine Pirolate Pitrazepin Pizotifen Profenamine Serazapine Siltenzepine Telenzepine Tipindole Tropatepine Zolenzepine

匿名

検索

案内

案内

pirenzepine